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1. 发明专利

IL258553D0 N-sulfonylated pyrazolo[3,4-b]pyridin-6-carboxamides and method of use 未知
公开(公告)号：IL258553D0
公开(公告)日：2018-05-31
申请号：IL25855318
申请日：2018-04-08
申请人： GALAPAGOS NV , ABBVIE SARL , AKKARI RHALID , ALVEY LUKE JONATHAN , BOCK XAVIER MARIE , BROWN BRIAN S , CLAES PIETER ISABELLE ROGER , COWART MARLON D , DE LEMOS ELSA , DESROY NICOLAS , DUTHION BERANGER , GFESSER GREGORY A , GOSMINI ROMAIN LUC MARIE , HOUSSEMAN CHRISTOPHER GAETAN , JANSEN KOEN KAREL , JI JIANGUO , KYM PHILIP R , LEFRANCOIS JEAN MICHEL , MAMMOLITI OSCAR , MENET CHRISTEL JEANNE MARIE , MERAYO NURIA MERAYO , NEWSOME GREGORY JOHN ROBERT , PALISSE ADELINE MARIE ELISE , PATEL SACHIN V , PIZZONERO MATHIEU RAFAEL , SHRESTHA ANURUPA , SWIFT ELIZABETH C , VAN DER PLAS STEVEN EMIEL , WANG XUEQING , DE BLIECK ANN
发明人： AKKARI RHALID , ALVEY LUKE JONATHAN , BOCK XAVIER MARIE , BROWN BRIAN S , CLAES PIETER ISABELLE ROGER , COWART MARLON D , DE LEMOS ELSA , DESROY NICOLAS , DUTHION BERANGER , GFESSER GREGORY A , GOSMINI ROMAIN LUC MARIE , HOUSSEMAN CHRISTOPHER GAETAN , JANSEN KOEN KAREL , JI JIANGUO , KYM PHILIP R , LEFRANCOIS JEAN-MICHEL , MAMMOLITI OSCAR , MENET CHRISTEL JEANNE MARIE , MERAYO NURIA MERAYO , NEWSOME GREGORY JOHN ROBERT , PALISSE ADELINE MARIE ELISE , PATEL SACHIN V , PIZZONERO MATHIEU RAFAEL , SHRESTHA ANURUPA , SWIFT ELIZABETH C , VAN DER PLAS STEVEN EMIEL , WANG XUEQING , DE BLIECK ANN
IPC分类号： C07D20060101
摘要： wherein R1, R2, R3, R4, R5, and R6 have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions mediated and modulated by CFTR, including cystic fibrosis, Sjögren's syndrome, pancreatic insufficiency, chronic obstructive lung disease, and chronic obstructive airway disease. Also provided are pharmaceutical compositions comprised of one or more compounds of formula (I).

2. 发明申请

WO02055496A8 ARYL PIPERIDINE AND PIPERAZINE DERIVATIVES AS INDUCERS OF LDL-RECEPTOR EXPRESSION 审中-公开
标题翻译：作为低密度脂蛋白受体表达的诱导剂的ARYL PIPERIDINE AND PIPERAZINE DERIVATIVES
公开(公告)号：WO02055496A8
公开(公告)日：2003-07-17
申请号：PCT/GB0100158
申请日：2001-01-15
申请人： GLAXO GROUP LTD , BOUILLOT ANNE MARIE JEANNE , BOMBRUN AGNES , DUMAITRE BERNARD ANDRE , GOSMINI ROMAIN LUC MARIE , RAMSDEN NIGEL GRAHAME , CONGREVE MILES STUART
发明人： BOUILLOT ANNE MARIE JEANNE , BOMBRUN AGNES , DUMAITRE BERNARD ANDRE , GOSMINI ROMAIN LUC MARIE , RAMSDEN NIGEL GRAHAME , CONGREVE MILES STUART
IPC分类号： C07D295/12 , A61K31/445 , A61K31/4468 , A61K31/451 , A61K31/4525 , A61K31/4535 , A61K31/454 , A61K31/4545 , A61K31/495 , A61K31/551 , A61P1/18 , A61P3/04 , A61P3/06 , A61P3/10 , A61P9/10 , A61P43/00 , C07D211/14 , C07D211/20 , C07D211/22 , C07D211/46 , C07D211/58 , C07D295/13 , C07D401/04 , C07D401/12 , C07D405/04 , C07D405/12 , C07D405/14 , C07D409/04 , C07D409/12 , C07D417/12
CPC分类号： C07D295/13 , A61K31/451 , A61K31/495 , C07D211/14 , C07D211/22 , C07D211/46 , C07D211/58 , C07D401/04 , C07D401/12 , C07D405/04 , C07D405/12 , C07D409/04 , C07D409/12
摘要： The invention concerns Use of a compound of formula (I) or a physiologically acceptable salt, solvate or derivative thereof, in the manufacture of a medicament for the treatment of diseases ameliorated by LDL-r upregulation, to novel compounds and pharmaceutical compositions within the scope of formula (I).
摘要翻译：本发明涉及式（I）化合物或其生理上可接受的盐，溶剂合物或衍生物在制备用于治疗LDL-r上调改善的疾病的药物中的用途，涉及范围内的新化合物和药物组合物的式（I）化合物。

3. 发明申请

WO02055495A8 ARYL PIPERIDINE DERIVATIVES AS INDUCERS OF LDL-RECEPTOR EXPRESSION 审中-公开
标题翻译：作为低密度脂蛋白受体表达诱导剂的ARYL PIPERIDINE衍生物
公开(公告)号：WO02055495A8
公开(公告)日：2003-07-17
申请号：PCT/GB0100155
申请日：2001-01-15
申请人： GLAXO GROUP LTD , BOUILLOT ANNE MARIE JEANNE , BOMBRUN AGNES , DUMAITRE BERNARD ANDRE , GOSMINI ROMAIN LUC MARIE , RAMSDEN NIGEL GRAHAME , CONGREVE MILES STUART
发明人： BOUILLOT ANNE MARIE JEANNE , BOMBRUN AGNES , DUMAITRE BERNARD ANDRE , GOSMINI ROMAIN LUC MARIE , RAMSDEN NIGEL GRAHAME , CONGREVE MILES STUART
IPC分类号： C07D211/14 , A61K31/445 , A61P1/18 , A61P3/06 , A61P3/10 , A61P9/00 , A61P9/10 , A61P43/00 , C07D211/22 , C07D211/34 , C07D401/06 , C07F9/59 , C07D211/26 , C07F9/12
CPC分类号： A61K31/445 , C07D211/22 , C07D211/34 , C07D401/06 , C07F9/592
摘要： The invention concerns a compound of formula (I), wherein Ar1 represents phenyl, naphthyl or phenyl fused by a C3-8cycloalkyl, where each group is substituted by a group -O-Z and optionally one to three further groups independently represented by R ; Ar2 represents phenyl or 5-6 membered heteroaromatic group, where each group is optionally substituted by one to four groups independently selected from halogen, C1-4 alkyl and C1-4 alkoxy; Ar3 represents a phenyl or a 5-6 membered heteroaromatic group, where each group is optionally substituted by one to four groups independently selected from hydroxy, alkyl, C1-4 alkoxy, C2-4 alkenyl, C2-4 alkenyloxy, C1-4 perfluoroalkoxy, C1-4 acylamino or an electron withdrawing group; A represents -C(H)-; E represents -C1-6 alkylene-; X represents -CON(H or C1-4alkyl)- or -N(H or C1-4alkyl)CO-;Y represents a direct link, -N(H or C1-4alkyl)CO- or -CON(H or C1-4alkyl)-; Z represents a metabolically labile group; R represents halogen, -S(C1-4alkyl)-, -O-(C0-4 alkylene)-R or -(C0-4alkylene)-R , where each alkylene group may additionally incorporate an oxygen in the chain, with the proviso that there are at least two carbon atoms between any chain heteroatoms; R represents: i) hydrogen, C1-4 perfluoroalkyl, C2-3alkenyl, ii) phenyl, naphthyl, a 5- or 6-membered heteroaromatic group or 1,2,3,4-tetrahydronaphthyl, optionally substituted by one or two halogen, hydroxy, C1-4 alkyl, C1-4 alkoxy groups, iii) C3-8cycloalkyl, a 3-7 membered heterocycloalkyl, iv) amino, C1-4 alkylamino or di-C1-4alkylamino, with the proviso that there are at least two carbon atoms between any chain heteroatoms;and physiologically acceptable salts, solvates and pharmaceutical compositions thereof and their use in treating disorders associated with elevated circulating levels of LDL-cholesterol.
摘要翻译：本发明涉及式（I）化合物，其中Ar 1表示苯基，萘基或被C 3-8环烷基稠合的苯基，其中每个基团被基团-OZ和任选地一个至三个另外由R 1独立地表示的基团取代。 ; Ar2表示苯基或5-6元杂芳基，其中每个基团任选被一至四个独立地选自卤素，C 1-4烷基和C 1-4烷氧基的基团取代; Ar 3表示苯基或5-6元杂芳基，其中各基团任选被一至四个独立地选自羟基，烷基，C 1-4烷氧基，C 2-4烯基，C 2-4链烯氧基，C 1-4全氟烷氧基，C 1-4酰基氨基或吸电子基团; A表示-C（H） - ; E表示-C 1-6亚烷基; X代表-CON（H或C 1-4烷基） - 或-N（H或C 1-4烷基）CO-; Y代表直链，-N（H或C 1-4烷基）CO-或-CON（H或C1- 1-4） - ; Z代表不稳定组; R 1表示卤素，-S（C 1-4烷基） - ， - O-（C 0-4亚烷基）-R 2或 - （C 0-4亚烷基）-R 2，其中每个亚烷基可另外包含链中的氧，条件是在任何链杂原子之间存在至少两个碳原子; R 2表示：i）氢，C 1-4全氟烷基，C 2-3烯基，ii）苯基，萘基，5或6元杂芳基或1,2,3,4-四氢萘基，任选地被一个或两个卤素，羟基，C 1-4烷基，C 1-4烷氧基，iii）C 3-8环烷基，3-7元杂环烷基，iv）氨基，C 1-4烷基氨基或二-C 1-4烷基氨基，条件是存在任何链状杂原子之间的至少两个碳原子;以及其生理上可接受的盐，溶剂化物和药物组合物，以及它们在治疗与升高的LDL-胆固醇循环水平相关的疾病中的用途。

4. 发明申请

WO0228859A3 CONDENSED PYRIDOINDOLE DERIVATIVES 审中-公开
标题翻译：浓缩的吡啶衍生物
公开(公告)号：WO0228859A3
公开(公告)日：2002-09-12
申请号：PCT/US0142173
申请日：2001-09-17
申请人： LILLY ICOS LLC , ORME MARK W , SAWYER JASON SCOTT , DAUGAN ALAIN CLAUDE-MARIE , GELLIBERT FRANCOISE , GOSMINI ROMAIN LUC MARIE
发明人： ORME MARK W , SAWYER JASON SCOTT , DAUGAN ALAIN CLAUDE-MARIE , GELLIBERT FRANCOISE , GOSMINI ROMAIN LUC MARIE
IPC分类号： A61K31/437 , A61K31/444 , A61K31/4545 , A61K31/496 , A61K31/5377 , A61P1/04 , A61P9/00 , A61P9/10 , A61P9/12 , A61P9/14 , A61P11/00 , A61P11/02 , A61P11/06 , A61P13/08 , A61P13/12 , A61P15/06 , A61P15/10 , A61P19/10 , A61P25/26 , A61P27/02 , A61P29/00 , A61P35/00 , A61P37/08 , A61P43/00 , C07D471/14
CPC分类号： C07D471/14
摘要： Compounds of the general structural formula (I) and use of the compounds and salts and solvates thereof, as therapeutic agents. In particular, the invention relates to compounds that, are potent and selective inhibitors of cyclic guanosine 3', 5'-monophosphate specific phosphodiesterase (cGMP-specific PDE), in particular PDE5, ad have utility in a variety of therapeutic areas wherein such inhibition is considered beneficial, including the treatment of cardiovascular disorders and erectile dysfunction.
摘要翻译：一般结构式（I）的化合物及其化合物及其盐和溶剂化物的用途作为治疗剂。特别地，本发明涉及作为环鸟嘌呤3'，5'-单磷酸特异性磷酸二酯酶（cGMP-特异性PDE），特别是PDE5的有效和选择性抑制剂的化合物，其可用于多种治疗领域，其中这种抑制被认为是有益的，包括治疗心血管疾病和勃起功能障碍。

5. 发明专利

CL2018000911A1 Pirazolo[3,4-b]piridin-6-carboxamidas n-sulfoniladas y método de uso 未知
公开(公告)号：CL2018000911A1
公开(公告)日：2018-08-24
申请号：CL2018000911
申请日：2018-04-09
申请人： ABBVIE SARL , GALAPAGOS NV
发明人： COWART MARLON D , VAN DER PLASS STEVEN EMIEL , WANG XUEQING , KYM PHILIP R , PATEL SACHIN V , AKKARI RHALID , ALVEY LUKE JONATHAN , BOCK XAVIER MARIE , BROWN BRIAN S , CLAES PIETER ISABELLE ROGER , DELEMOS ELSA , DESROY NICOLAS , DUTHION BÉRANGER , GFESSER GREGORY A , GOSMINI ROMAIN LUC MARIE , HOUSSEMAN CHRISTOPHER GAËTAN , JANSEN KOEN KAREL , JI JIANGUO , LEFRANCOIS JEAN-MICHEL , MAMMOLITI OSCAR , MENET CHRISTEL JEANNE MARIE , MERAYO NURIA MERAYO , NEWSOME GREGORY JOHN ROBERT , PALISSE ADELINE MARIE ELISE , PIZZONERO MATHIEU RAFAËL , SHRESTHA ANURUPA , SWIFT ELIZABETH C , DE BLIECK ANN
IPC分类号： A61K31/437 , A61P11/12 , C07D471/04 , C07D519/00
摘要： La presente invención proporciona compuestos de fórmula (I)) en donde R1, R2, R3, R4, R5 y R6 tiene cualquiera de los valores definidos en la memoria descriptiva, y sales farmacéuticamente aceptables de los mismos, que son útiles como agentes en el tratamiento de enfermedades y afecciones mediadas y moduladas por CFTR, que incluyen fibrosis quística, síndrome de Sjögren, insuficiencia pancreática, enfermedad pulmonar obstructiva crónica y enfermedad obstructiva crónica de las vías aéreas. También se proporcionan composiciones farmacéuticas comprendidas por uno o más compuestos de fórmula (I).

6. 发明专利

SG11201802932VA N-SULFONYLATED PYRAZOLO[3,4-B]PYRIDIN-6-CARBOXAMIDES AND METHOD OF USE 未知
公开(公告)号：SG11201802932VA
公开(公告)日：2018-05-30
申请号：SG11201802932V
申请日：2016-10-07
申请人： ABBVIE SARL , GALAPAGOS NV
发明人： AKKARI RHALID , ALVEY LUKE JONATHAN , BOCK XAVIER MARIE , BROWN BRIAN S , CLAES PIETER ISABELLE ROGER , COWART MARLON D , DE LEMOS ELSA , DESROY NICOLAS , DUTHION BÉRANGER , GFESSER GREGORY A , GOSMINI ROMAIN LUC MARIE , HOUSSEMAN CHRISTOPHER GAËTAN , JANSEN KOEN KAREL , JI JIANGUO , KYM PHILIP R , LEFRANCOIS JEAN-MICHEL , MAMMOLITI OSCAR , MENET CHRISTEL JEANNE MARIE , MERAYO NURIA MERAYO , NEWSOME GREGORY JOHN ROBERT , PALISSE ADELINE MARIE ELISE , PATEL SACHIN V , PIZZONERO MATHIEU RAFAËL , SHRESTHA ANURUPA , SWIFT ELIZABETH C , VAN DER PLAS STEVEN EMIEL , WANG XUEQING , DE BLIECK ANN
IPC分类号： C07D471/04 , A61K31/437 , A61P11/12 , C07D519/00
摘要： wherein R1, R2, R3, R4, R5, and R6 have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions mediated and modulated by CFTR, including cystic fibrosis, Sjögren's syndrome, pancreatic insufficiency, chronic obstructive lung disease, and chronic obstructive airway disease. Also provided are pharmaceutical compositions comprised of one or more compounds of formula (I).

7. 发明专利

AU2016333907A1 Novel compounds for treatment of cystic fibrosis 未知
公开(公告)号：AU2016333907A1
公开(公告)日：2018-04-12
申请号：AU2016333907
申请日：2016-10-07
申请人： ABBVIE SARL , GALAPAGOS NV
发明人： AKKARI RHALID , ALVEY LUKE JONATHAN , BOCK XAVIER MARIE , BROWN BRIAN S , CLAES PIETER ISABELLE ROGER , COWART MARLON D , CONRATH KATJA E , CYR DOUGLAS , DE LEMOS ELSA , DE WILDE GERT JULES HECTOR , DESROY NICOLAS , DUTHION BERANGER , GFESSER GREGORY A , GOSMINI ROMAIN LUC MARIE , HOUSSEMAN CHRISTOPHER GAETAN , JANSEN KOEN KAREL , JI JIANGUO , KYM PHILIP R , LEFRANCOIS JEAN-MICHEL , MAMMOLITI OSCAR , MENET CHRISTEL JEANNE MARIE , MERAYO NURIA MERAYO , NEWSOME GREGORY JOHN ROBERT , PALISSE ADELINE MARIE ELISE , PATEL SACHIN V , PIZZONERO MATHIEU RAFAEL , SHRESTHA ANURUPA , SWIFT ELIZABETH C , TSE CHRIS , VAN DER PLAS STEVEN EMIEL , WANG XUEQING
IPC分类号： C07D471/04 , A61K31/437 , A61P11/00 , C07D519/00 , G01N33/68
摘要： A corrector agent capable of stabilizing a newly synthesized cystic fibrosis transmembrane conductance regulator (CFTR) protein, useful in the treatment of cystic fibrosis.

10. 发明专利

PH12018500765A1 N-SULFONYLATED PYRAZOLO[3,4-B]PYRIDIN-6-CARBOXAMIDES AND METHOD OF USE 未知
公开(公告)号：PH12018500765A1
公开(公告)日：2018-10-01
申请号：PH12018500765
申请日：2018-04-06
申请人： ABBVIE SARL , GALAPAGOS NV
发明人： AKKARI RHALID , ALVEY LUKE JONATHAN , BOCK XAVIER MARIE , BROWN BRIAN S , CLAES PIETER ISABELLE ROGER , COWART MARLON D , DE LEMOS ELSA , DESROY NICOLAS , DUTHION BERANGER , GFESSER GREGORY A , GOSMINI ROMAIN LUC MARIE , HOUSSEMAN CHRISTOPHER GAETAN , JANSEN KOEN KAREL , JI JIANGUO , KYM PHILIP R , LEFRANCOIS JEAN-MICHEL , MAMMOLITI OSCAR , MENET CHRISTEL JEANNE MARIE , MERAYO NURIA MERAYO , NEWSOME GREGORY JOHN ROBERT , PALISSE ADELINE MARIE ELISE , PATEL SACHIN V , PIZZONERO MATHIEU RAFAEL , SHRESTHA ANURUPA , SWIFT ELIZABETH C , VAN DER PLAS STEVEN EMIEL , WANG XUEQING , DE BLIECK ANN
IPC分类号： A61K31/437 , A61P11/12 , C07D471/04 , C07D519/00
摘要： The present invention provides for compounds of formula (I) wherein R1, R2, R3, R4, R5, and R6 have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions mediated and modulated by CFTR, including cystic fibrosis, Sjogren's syndrome, pancreatic insufficiency, chronic obstructive lung disease, and chronic obstructive airway disease. Also provided are pharmaceutical compositions comprised of one or more compounds of formula (I).

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